Generic
Tenofovir Alafenamide
8 brands available in the market
At a glance
Tenofovir Alafenamide is a nucleotide reverse transcriptase inhibitor (NRTI) used for the treatment of chronic hepatitis B virus (HBV) infection. It inhibits HBV replication.
Description
Tenofovir Alafenamide is a phosphonamidate prodrug of tenofovir that enters primary hepatocytes via passive diffusion and OATP1B1/OATP1B3 transporters, and is converted to tenofovir by carboxylesterase 1. Tenofovir is phosphorylated to tenofovir diphosphate, which incorporates into viral DNA by HBV reverse transcriptase, causing DNA chain termination.
Indications
- Chronic hepatitis B (HBV) infection (compensated liver disease, adults)
Therapeutic class
Hepatic Viral Infections (Hepatitis B)
Pharmacological class
Nucleotide Reverse Transcriptase Inhibitor (NRTI)
Pharmacology
Tenofovir Alafenamide enters hepatocytes via OATP1B1/OATP1B3 and is converted to tenofovir by carboxylesterase 1. Tenofovir diphosphate is incorporated into viral DNA by HBV reverse transcriptase, causing DNA chain termination and inhibiting HBV replication.
Mechanism of action
Inhibits HBV reverse transcriptase to stop viral replication.
Dosage
Adult Dose (Oral):
- 25 mg tablet once daily with food
- Renal impairment (eGFR ≥15 mL/min or ESRD on hemodialysis): No dose adjustment needed; administer after dialysis
- Hepatic impairment (Child-Pugh A): No dose adjustment; decompensated (Child-Pugh B/C): Not recommended
Administration
- Take with food
- Swallow tablet whole; do not chew, crush, or break
- Take at the same time each day
Missed dose
If you miss a dose, take it as soon as you remember; if almost time for the next dose, skip it; do not double the dose.
Side effects
Common Side Effects:
- Headache
- Abdominal pain
- Fatigue, cough, nausea
- Back pain
Serious:
- Lactic acidosis/severe hepatomegaly with steatosis
- Renal impairment
- Severe exacerbation of hepatitis B (upon treatment discontinuation)
Precautions & warnings
- Do not use alone in HIV-1 coinfected patients (risk of HIV-1 resistance)
- Severe exacerbation of hepatitis B may occur upon discontinuation; monitor for several months after stopping
- New onset or worsening renal impairment: Monitor serum creatinine, eGFR, urine glucose and protein
- Suspend if lactic acidosis is suspected
Contraindications
- Hypersensitivity to tenofovir alafenamide
Drug interactions
- P-gp/BCRP inducers (carbamazepine, phenytoin, rifampin): Decrease tenofovir alafenamide absorption and plasma concentrations
- P-gp/BCRP inhibitors: Increase absorption and plasma concentrations
- Drugs eliminated by active tubular secretion (acyclovir, aminoglycosides, NSAIDs): Increase tenofovir concentrations
Food interactions
It is not known whether alcohol is safe with Tenofovir Alafenamide; consult your doctor.
Use in pregnancy
Use in Pregnancy: Generally safe; animal studies show low or no adverse effects; limited human data; consult your doctor.
Pregnancy Category: B — always consult a doctor before taking during pregnancy.
Use in lactation
Use in Lactation: Probably safe; limited data suggests no significant risk; consult your doctor.
Pediatric use
Safety and efficacy not established in children <18 years
Geriatric use
No clinically significant differences between elderly and younger subjects
Renal / hepatic impairment
Renal Impairment: eGFR ≥15 or ESRD on dialysis: no dose adjustment; ESRD without dialysis: not recommended; consult your doctor.
Hepatic Impairment: Mild (Child-Pugh A): no dose adjustment; decompensated (Child-Pugh B/C): not recommended; consult your doctor.
Overdose effects
In overdose, provide general supportive measures and monitor vital signs; tenofovir is removed by hemodialysis (extraction coefficient approximately 54%).
Storage conditions
Store below 30°C in the original container, protected from light; keep out of reach of children.
Chemical structure
Tenofovir Alafenamide